4,5-DIHYDRO-4-OXO-3H-IMIDAZO[4,5-C]PYRIDINES - POTENT ARYLACETIC ACID-DERIVED AT(1) ANTAGONISTS WITH IMPROVED AFFINITY FOR THE AT(2) RECEPTOR

Authors
MEDERSKI WWKR DORSCH D OSSWALD M BEIER N LUES I MINCK KO SCHELLING P LADSTETTER BJ
Citation
Wwkr. Mederski et al., 4,5-DIHYDRO-4-OXO-3H-IMIDAZO[4,5-C]PYRIDINES - POTENT ARYLACETIC ACID-DERIVED AT(1) ANTAGONISTS WITH IMPROVED AFFINITY FOR THE AT(2) RECEPTOR, Bioorganic & medicinal chemistry letters, 5(22), 1995, pp. 2665-2670
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
22
Year of publication
1995
Pages
2665 - 2670
Database
ISI
SICI code
0960-894X(1995)5:22<2665:4-PAA>2.0.ZU;2-4
Abstract
The replacement of dimethylacetamide with arylacetic acid esters and a cetamides at the imidazo[4,5-c]pyridine 5-position of EMD 66684 2 impa rts affinity for the AT(2) receptor. The highest affinity was found wi th the phenylacetic acid isopropylester moiety, which led to compound 7c with an IC50 value of 32 nM (AT(2)) and an AT(2)/AT(1) ratio of 5.